FINSAVA

Quick Overview

Our aim is to reach out to the globe within shortest possible time frame.

To promote this objective, not only we distribute and market our Male Health range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Finsava which contains Finasteride USP 1 mg .

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Details

Each Film-Coated tablet contains:

Finasteride USP….1 mg

Excipients q.s

Colour : Titanium dioxide BP

Chemical Name

4-Azaandrost-1-ene-17-carboxamide, N-(1,1-dimethylethyl)-3-oxo-,

(5a ,1 713 )-.

Category

Finasteride, a synthetic 4-azasteroid compound, is a specific inhibitor of steroid Type ll 5a-reductase, an intracellular enzyme that converts the androgen testosterone into 5a-di hydrotestosterone (DHT).

DESCRIPTION

White to off white film-coated round shaped tablets plain on both side.

CLINICAL PHARMACOLOGY

Finasteride is a competitive and specific inhibitor of Type ll 5a­reductase, an intracellular enzyme that converts the androgen testosterone into DHT.

In humans, the mechanism of action of Finasteride is based on its preferential inhibition of the Type II lsozyme. Using native tissues (scalp and prostate), in vitro binding studies examining the potential of Finasteride to inhibit either of the Isozymes, revealed a 100-fold selectivity for the human Type ll 5a-reductase over Type I lsozyme (IC50=500 and 4.2 nM for Type I and II, respectively). For both lsozymes, the inhibition by Finasteride is accompanied by reduction of the inhibitor to Dihydrofinasteride and adducts formation with NADP+. The turnover for the enzyme complex is slow (t1/2 approximately 30 days for the Type II enzyme complex and 14 days for the Type I complex).

Finasteride has no affinity for the androgen receptor and has no Androgenic, Antindrogenic, Estrogenic, Antiestrogenic, or Progestational effects. Inhibltion of Type ll 5a-reductase blocks the peripheral conversion of testosterone to DHT, resulting in significant decreases in serum and tissue DHT concentrations. Finasteride produces a rapid reduction in serum DHT concentration, reaching 65% suppression within 24 hours of oral dosing with a lmg tablet. Mean circulating levels of Testosterone and Estradiol were increased by approximately 15% as compared to baseline, but these remained within the physiological range.

In men with male pattern hair loss (Androgenetic Alopecia), the balding scalp contains miniaturized hair follicles and increased amounts of DHT compared with hairy scalp. Administration of Finasteride decreases scalp and serum DHT concentrations in these men. The relative contributions of these reductions to the treatment effect of Finasteride have not been defined. By this mechanism, Finasteride appears to interrupt a key factor in the development of Androgenetic Alopecia in those patients genetically predisposed.

PHARMACOKINETICS

Absorption

In a study in 15 healthy young male subjects, the mean bioavailability of Finasteride lmg tablets was 65% (range 26-170%), based on the ratio of area under the curve (AUC) relative to an intravenous (IV) reference dose. At steady state following dosing with 1 mg/day (n=12), maximum Finasteride plasma concentration averaged 9.2 ng/mL (range, 4.9-13.7 ng/mL) and was reached 1 to 2 hours post-dose; AUC (0-24 hr) was 53 ng • hr/mL (range, 20-154 ng • hr/mL). Bioavailability of Finasteride was not affected by food.

Metabolism

Finasteride is extensively metabolized in the liver, primarily via the Cytochrome P450 3A4 enzyme subfamily. Two metabolites, the t-butyl side chain Monohydroxylated and Monocarboxylic acid metabolites, have been identified that possess no more than 20% of the 5a­reductase inhibitory activity of Finasteride.

Excretion

Following intravenous infusion in healthy young subjects (n=15), mean plasma clearance of Finasteride was 165 mi./min (range, 70-279 mi./min). Mean terminal half-life in plasma was 4.5 hours (range, 3.3- 13.4hours; n=12). Following an oral dose of 14C-finasteride in man (n=6), a mean of 39% (range, 32-46%) of the dose was excreted in the urine in the form of metabolites; 57% (range, 51-64%) was excreted in the feces.

Mean terminal half-life is approximately 5-6 hours in men 18-60 years of age and 8 hours in men more than 70 years of age.

Special Populations

Pediatric: Finasteride pharmacokinetics have not been investigated in patients <18 years of age.

Gender: FINSAVA is not indicated for use in women.

Geriatric: No dosage adjustment is necessary in the elderly. Although the elimination rate of Finasteride is decreased in the elderly, these findings are of no clinical significance.

Race: The effect of race on Finasteride pharmacokinetics has not been studied.

Renal Insufficiency: No dosage adjustment is necessary in patients with renal insufficiency.

Hepatic Insufficiency: The effect of hepatic insufficiency on Finasteride pharmacokinetics has not been studied. Caution should be used in the administration of FINSAVA in patients with liver function abnormalities, as Finasteride is metabolized extensively in the liver.

DRUG INTERACTION

No drug interactions of clinical importance have been identified. Finasteride does not appear to affect the Cytochrome P450-linked drug-metabolizing enzyme system.

INDICATION

FINSAVA is indicated for the treatment of male pattern hair loss (Androgenetic Alopecia) on the vertex and the anterior mid-scalp area in MEN ONLY.

CONTRAINDICATION

Finasteride is contraindicated in the following:

Pregnancy: Finasteride use is contraindicated in women when they are or may potentially be pregnant. Because of the ability of Type II 5a­reductase inhibitors to inhibit the conversion of testosterone to DHT, Finasteride may cause abnormalities of the external genitalia of a male fetus of a pregnant woman who receives Finasteride. If this drug is used during pregnancy, or if pregnancy occurs while taking this drug, the pregnant woman should be apprised of the potential hazard to the male fetus.

WARNINGS

Finasteride is not indicated in children and women.

EXPOSURE OF WOMEN - RISK TO MALE FETUS

Crushed or broken tablets must not be handled by women, who are pregnant or may become pregnant because of the possibility of absorption of Finasteride and the subsequent potential risk to a male fetus.

PRECAUTIONS

General

Caution should be used in the administration of Finasteride in patients with liver function abnormalities, as Finasteride is metabolized extensively in the liver.

Physicians

Physicians should instruct their patients to promptly report any changes in their breasts such as lumps, pain or nipple discharge. Breast changes including breast enlargement, tenderness and neoplasm have been reported.

Patients

Finasteride can affect a blood test called PSA (Prostate-Specific Antigen) for the screening of prostate cancer. If you have a PSA test done, you should tell your doctor(s) that you are taking Finasteride. Because Finasteride decreases PSA levels, changes in PSA levels will need to be carefully evaluated by your doctor(s). Any increase in follow-up PSA levels from their lowest point should be carefully evaluated even if the test results are still within the normal range for men not taking Finasteride. You should also tell your doctor if you have not been taking Finasteride as prescribed because this may affect the PSA test results. For more information, talk to your doctor.

Nursing Mothers

Finasteride is not indicated for use in women.

It is not known whether Finasteride is excreted in human milk.

Pediatric Use

Finasteride is not indicated for use in pediatric patients.

Safety & effectiveness in pediatric patients have not been established.

SIDE EFFECTS

Like all prescription products, Finasteride may cause side effects. In clinical studies, side effects from Finasteride were uncommon and did not affect most men. A small number of men experienced certain sexual side effects.

These men reported one or more of the following: less desire for sex; difficulty in achieving an erection; and, a decrease in the amount of semen. Each of these side effects occurred in less than 2% of men. These side effects went away in men who stopped taking Finasteride. They also disappeared in most men who continued taking Finasteride. In general use, the following have been reported: allergic reactions including rash, itching, hives and swelling of the lips and face; problems with ejaculation; breast tenderness and enlargement; depression; and testicular pain. You should promptly report to your doctor any changes in your breasts such as lumps, pain or nipple discharge.

DOSAGE AND ADMINISTRATION

The recommended dosage is 1 mg orally once a day.

FINSAVA may be administered with or without meals.

In general, daily use for three months or more is necessary before benefit is observed. Continued use is recommended to sustain benefit, which should be re-evaluated periodically. Withdrawal of treatment leads to reversal of effect whin 12 months.

PRESENTATION. Blister of 10 tablets

STORAGE & HANDLING.

Store in a cool, dry place below 30°C . Keep out of reach of children.